Identification of trichostatin derivatives from Streptomyces sp. CPCC 203909

  • Bioorg Med Chem Lett. 2015 Feb 1;25(3):562-5. doi: 10.1016/j.bmcl.2014.12.030.
Minghua Chen  1 ,  Yexiang Wu  1 ,  Yi He  2 ,  Yanni Xu  1 ,  Yongzhen Li  1 ,  Dongsheng Li  1 ,  Tingting Feng  1 ,  Liyan Yu  1 ,  Bin Hong  1 ,  Wei Jiang  3 ,  Shuyi Si  4
Affiliations
  • 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.
  • 2. Information Center, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100730, People's Republic of China.
  • 3. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China. Electronic address: [email protected].
  • 4. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China. Electronic address: [email protected].
PMID: 25556102 DOI: 10.1016/j.bmcl.2014.12.030
Abstract

Four new trichostatin analogues (1-4) and six known analogues have been isolated from the rice fermentation of the Streptomyces sp. CPCC 203909. The structures and absolute configurations of these compounds were determined by extensive spectroscopic analysis including 2D NMR and electronic circular dichroism (ECD) calculations based on the quantum-mechanical time-dependent density functional theory (TDDFT). Compounds 2, 5-7, 9, and 10 up-regulated the transcriptional activity of human high density lipoprotein receptor (CLA-1) with EC50 values of 0.38-78.83μM.

Keywords
Atherosclerosis; Human high density lipoprotein receptor; Streptomyces sp.; Trichostatin analogues.